Entrectinib CAS 1108743-60-7
TRK / ROS1 / ALK Tyrosine Kinase Inhibitor (CNS-Active)
Entrectinib (CAS 1108743-60-7), also RXDX-101, is a potent, CNS-active inhibitor of the TRKA/B/C, ROS1 and ALK tyrosine kinases. It blocks oncogenic fusions driving NTRK-, ROS1- and ALK-rearranged tumors, inducing regression across tissue-agnostic indications (approved as Rozlytrek). Formula C31H34F2N6O2, MW 560.6. Research-grade with COA.
Molecular Information
CAS: 1108743-60-7
Formula: C31H34F2N6O2
MW: 560.6 g/mol
Class: TRK/ROS1/ALK TKI
Core: Indazole benzamide piperazine
Target: TRKA/B/C, ROS1, ALK
Activity: Oncogenic-fusion blockade
MP: Not firmly reported
Appearance: White to off-white powder
Synonyms: RXDX-101
Storage: -20°C, protect from light
Product Technical Specifications
Complete physicochemical properties and QC parameters for Entrectinib (CAS 1108743-60-7)
📋 Physicochemical Properties
- Product NameEntrectinib (RXDX-101)
- IUPAC NameN-[5-[(3,5-difluorophenyl)methyl]-1H-indazol-3-yl]-4-(4-methylpiperazin-1-yl)-2-(oxan-4-ylamino)benzamide
- CAS Number1108743-60-7
- SynonymsEntrectinib; RXDX-101
- Molecular FormulaC31H34F2N6O2
- Molecular Weight560.6 g/mol
- SourceSynthetic kinase inhibitor
- AppearanceWhite to off-white powder
- Water SolubilityLow
- Organic SolubilityDMSO; some aqueous buffers
- Compound ClassTRK/ROS1/ALK tyrosine kinase inhibitor
- HS Code2934.99
🔬 Quality Control & Handling
- Purity (HPLC)≥98%
- FormCrystalline powder
- Primary TargetTRKA/B/C, ROS1, ALK
- Assay ReadoutPhospho-kinase; tumor regression
- SelectivityPan-TRK + ROS1 + ALK; CNS-penetrant
- Storage Condition-20°C, sealed, protect from light
- Solution StabilityDMSO stock stable weeks at -20°C
- ShippingCold chain recommended
- QC DocumentationCOA / HPLC / NMR / MS / MSDS
- Pack Sizes100mg / 500mg / 1g / 5g / 10g
- Stock StatusIn Stock
- Use StatementResearch / investigational; not for human use
Key Molecular Targets & Pathway Nodes
Entrectinib engages the molecular machinery and pathway nodes that define its research utility.
How Entrectinib Works: Silencing Fusion-Driven Kinases
Entrectinib blocks TRK/ROS1/ALK kinases, shutting down the signals that drive fusion-positive tumors
Inhibition of TRK / ROS1 / ALK Kinase Domains
Entrectinib is a small-molecule TKI that occupies the ATP-binding pockets of TRKA/B/C, ROS1 and ALK, preventing their phosphorylation and activation.
Suppression of Oncogenic Fusion Signaling
In NTRK-, ROS1- or ALK-rearranged cancers, these fusions constitutively drive MAPK/PI3K and proliferative signaling; entrectinib interrupts that cascade.
Tumor Regression & CNS Activity
Blockade halts proliferation and induces regression across tumor types regardless of tissue origin (tissue-agnostic), and its CNS penetration addresses brain metastases.
⚖️ Entrectinib vs Comparators
- Entrectinib (this product)Pan-TRK + ROS1 + ALK; CNS-active
- LarotrectinibSelective TRK inhibitor
- CrizotinibROS1/ALK (less TRK) inhibitor
- Selective EdgeBroad TRK/ROS1/ALK + brain penetration
- Research NicheNTRK/ROS1/ALK fusion oncology
♻️ Downstream Biological Consequences
- KinaseTRK/ROS1/ALK inhibited
- PathwayMAPK/PI3K suppressed
- ProliferationGrowth arrested
- TumorRegression in fusions
- CNSBrain metastases addressed
- BiomarkerNTRK/ROS1/ALK testing
Research Applications & Models
Entrectinib is the reference pan-TRK/ROS1/ALK inhibitor for fusion-driven oncology.
NTRK Fusion Oncology
Benchmark pan-TRK inhibitor for tissue-agnostic NTRK-rearranged tumors.
NTRKROS1+ NSCLC Models
Studied in ROS1-rearranged non-small-cell lung cancer.
ROS1ALK+ Tumors
Evaluated in ALK-positive malignancies.
ALKTissue-Agnostic Cancer Research
Driven by genomic alteration, not tumor site.
Tissue-agnosticKinase Profiling
TRK/ROS1/ALK selectivity and panel screening.
KinaseCNS Penetration Studies
Brain-metastasis and intracranial models.
CNSKey Literature & Landmark Publications
Landmark work on entrectinib and TRK/ROS1/ALK fusion inhibition.
Available Sizes & Ordering
Research-grade Entrectinib / RXDX-101 (CAS 1108743-60-7) with full QC documentation; standard packs and bulk custom quantities supported.
| Tier | Pack Size | Stock Status | Suitable For | Lead Time |
|---|---|---|---|---|
| Standard | 100mg | In Stock | Kinase / oncology assays | Same/next-day ship |
| Medium | 500mg | In Stock | Cell & fusion studies | Same/next-day ship |
| Large | 1g | In Stock | In vivo tumor models | Same/next-day ship |
| Bulk | 5g | In Stock | Screening & formulation | Quote to confirm |
| Industrial | 10g+ | Made to order | Process development | Batch delivery |
💡 Reference sizes shown above; for exact pricing and availability please contact us for a quote. Bulk orders qualify for tiered discounts.
Frequently Asked Questions (FAQ)
What is entrectinib and what does it inhibit?
Why is entrectinib called tissue-agnostic?
Which cancers is it studied in?
What readouts confirm activity?
How soluble is entrectinib and how should it be prepared?
Is QC documentation provided?
Need Entrectinib for Your Research?
Research-grade Entrectinib (CAS 1108743-60-7) — purity ≥98% HPLC, COA included
Pan-TRK / ROS1 / ALK Inhibitor — request a quote today




